Plasma and Intrapulmonary Pharmacokinetics of Ceftibuten and Ledaborbactam in Healthy Male and Female Participants 18 to ≤55 Years of Age

Phase 1

Completed

• Conditions: Pharmacokinetics; Healthy Volunteers
• Interventions: Drug: ledaborbactam etzadroxil; Drug: ceftibuten

• Registration Number: NCT06665555
• Lead Sponsor: Venatorx Pharmaceuticals, Inc.

Brief Summary

This is a Phase 1, open-label, single-center PK study in healthy adult male and female participants between 18 and 55 years of age (both inclusive). Thirty-one participants will each undergo one standard bronchoscopy with bronchoalveolar lavage (BAL) following the fifth dose of ceftibuten-ledaborbactam etzadroxil or ceftibuten alone. BAL fluid samples and plasma samples will be collected at designated timepoints to determine the concentrations of ceftibuten, ledaborbactam, and urea.

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2024-10-29
• Study First Submitted QC: 2024-10-29
• Study First Posted: 2024-10-30
• Status Verified: 2024-11
• Study Start: 2024-11-04
• Primary Completion: 2025-03-13
• Study Completion: 2025-03-17
• Last Update Submitted: 2025-03-20
• Last Update Posted: 2025-03-25

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 34

Inclusion Criteria

• Healthy adults 18-55 years
• Males or non-pregnant, non-lactating females
• Body Mass Index: ≥18 and ≤32 kg/m2
• Forced expiratory volume in 1 second of at least 80% of predicted value
• Laboratory values meeting defined entry criteria

Exclusion Criteria

• History of drug allergy or hypersensitivity to penicillin, cephalosporin, or β-lactam antibacterial drug or to medications used during a bronchoscopy
• Conditions that potentially alter absorption and/or excretion of orally administered drugs
• History or presence of significant diseases, including any clinically relevant acute illness or surgery within the past 3 months
• Positive alcohol, drug, or tobacco use/test

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
Group 1	ledaborbactam etzadroxil	Participants in Group 1 will undergo one standardized bronchoscopy with bronchoalveolar lavage after the fifth dose of ceftibuten-ledaborbactam etzadroxil.
Group 1	ceftibuten	Participants in Group 1 will undergo one standardized bronchoscopy with bronchoalveolar lavage after the fifth dose of ceftibuten-ledaborbactam etzadroxil.
Group 2	ceftibuten	Participants in Group 2 will undergo one standardized bronchoscopy with bronchoalveolar lavage after the fifth of dose of ceftibuten alone.

Primary Outcome Measures

Name	Time	Method
Intrapulmonary PK - AUC0-12 (ledaborbactam)	0-12 hours after 5th dose	Area under the curve from time zero to 12 hours
Plasma PK - Cmax (ceftibuten)	0-12 hours after 5th dose	Maximum concentration
Plasma PK - Cmax (ledaborbactam)	0-12 hours after 5th dose	Maximum concentration
Plasma PK - AUC0-12 (ceftibuten)	Time Frame: 0-12 hours after 5th dose	Area under the curve from time zero to 12 hours
Plasma PK - AUC0-12 (ledaborbactam)	0-12 hours after 5th dose	Area under the curve from time zero to 12 hours
Intrapulmonary PK - AUC0-12 (ceftibuten)	0-12 hours after 5th dose	Area under the curve from time zero to 12 hours
Ratios of drug exposure in ELF to plasma using the AUC values for each matrix	0-12 hours after 5th dose

Secondary Outcome Measures

Name	Time	Method
Proportion of participants experiencing treatment-emergent adverse events (TEAEs) and serious adverse events (SAEs)	Day 1 - Day 8
Proportion of participants discontinuing study drug due to TEAEs and SAEs	Day 1 - Day 8

Trial Locations

Locations (1)

Pulmonary Associates; 🇺🇸 Phoenix, Arizona, United States